https://scholars.lib.ntu.edu.tw/handle/123456789/502884
DC 欄位 | 值 | 語言 |
---|---|---|
dc.contributor.author | HAO-CHIEH CHIU | en_US |
dc.contributor.author | Lee S.-L. | en_US |
dc.contributor.author | Kapuriya N. | en_US |
dc.contributor.author | Wang D. | en_US |
dc.contributor.author | Chen Y.-R. | en_US |
dc.contributor.author | SUNG-LIANG YU | en_US |
dc.contributor.author | Kulp S.K. | en_US |
dc.contributor.author | LEE-JENE TENG | en_US |
dc.contributor.author | Chen C.-S. | en_US |
dc.creator | Chiu H.-C.;Lee S.-L.;Kapuriya N.;Wang D.;Chen Y.-R.;Sung-Liang Yu;Kulp S.K.;Teng L.-J.;Chen C.-S. | - |
dc.date.accessioned | 2020-06-17T03:01:47Z | - |
dc.date.available | 2020-06-17T03:01:47Z | - |
dc.date.issued | 2012 | - |
dc.identifier.issn | 0968-0896 | - |
dc.identifier.uri | https://scholars.lib.ntu.edu.tw/handle/123456789/502884 | - |
dc.description.abstract | Methicillin-resistant Staphylococcus aureus (MRSA) poses a serious threat to public health because of its resistance to multiple antibiotics most commonly used to treat infection. In this study, we report the unique ability of the cyclooxygenase-2 (COX-2) inhibitor celecoxib to kill Staphylococcus aureus and MRSA with modest potency. We hypothesize that the anti-Staphylococcus activity of celecoxib could be pharmacologically exploited to develop novel anti-MRSA agents with a distinct mechanism. Examination of an in-house, celecoxib-based focused compound library in conjunction with structural modifications led to the identification of compound 46 as the lead agent with high antibacterial potency against a panel of Staphylococcus pathogens and different strains of MRSA. Moreover, this killing effect is bacteria-specific, as human cancer cells are resistant to 46. In addition, a single intraperitoneal administration of compound 46 at 30 mg/kg improved the survival of MRSA-infected C57BL/6 mice. In light of its high potency in eradicating MRSA in vitro and its in vivo activity, compound 46 and its analogues warrant continued preclinical development as a potential therapeutic intervention against MRSA. ? 2012 Elsevier Ltd. All rights reserved. | - |
dc.relation.ispartof | Bioorganic and Medicinal Chemistry | - |
dc.subject.classification | [SDGs]SDG3 | - |
dc.subject.other | 4 (5 anthracen 9 yl 3 trifluoromethyl pyrazol 1 yl)benzamide; amoxicillin; ampicillin; antiinfective agent; celecoxib; chloramphenicol; n [4 (5 anthracen 2 yl 3 trifluoromethyl pyrazol 1 yl)phenyl]aminosulfonamide; n [4 (5 anthracen 9 yl 3 trifluoromethyl pyrazol 1 yl) phenyl]aminosulfonamide; n [4 (5 biphenyl 4 yl 3 trifluoromethyl pyrazol 1 yl) phenyl]aminosulfonamide; n [4 (5 naphthalen 2 yl 3 trifluoromethyl pyrazol 1 yl)phenyl]aminosulfonamide; n [4 (5 para tolyl 3 trifluoromethyl pyrazol 1 yl) phenyl]aminosulfonamide; n [4 (5 phenanthren 2 yl 3 trifluoromethyl pyrazol 1 yl)phenyl] aminosulfonamide; n [4 [5 (4' bromobiphenyl 4 yl) 3 trifluoromethyl pyrazol 1 yl]phenyl]aminosulfonamide; n [4 [5 (4' methylbiphenyl 4 yl) 3 trifluoromethyl pyrazol 1 yl]phenyl]aminosulfonamide; unclassified drug; animal experiment; animal model; antibacterial activity; article; bacterial strain; cancer cell; chemical modification; drug efficacy; drug potency; drug research; drug structure; drug synthesis; female; human; human cell; in vitro study; in vivo study; methicillin resistant Staphylococcus aureus; methicillin resistant Staphylococcus aureus infection; molecular library; mouse; nonhuman; single drug dose; species differentiation; Staphylococcus aureus; Animals; Anti-Bacterial Agents; Antineoplastic Agents; Cell Proliferation; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Female; HT29 Cells; Humans; Injections, Intraperitoneal; Methicillin-Resistant Staphylococcus aureus; Mice; Mice, Inbred C57BL; Microbial Sensitivity Tests; Molecular Structure; Structure-Activity Relationship; methicillin resistant Staphylococcus aureus; Mus; Staphylococcus; Staphylococcus aureus | - |
dc.title | Development of novel antibacterial agents against methicillin-resistant Staphylococcus aureus | en_US |
dc.type | journal article | en |
dc.identifier.doi | 10.1016/j.bmc.2012.06.018 | - |
dc.identifier.pmid | 22750009 | - |
dc.identifier.scopus | 2-s2.0-84863985411 | - |
dc.relation.pages | 4653-4660 | - |
dc.relation.journalvolume | 20 | - |
dc.relation.journalissue | 15 | - |
item.fulltext | no fulltext | - |
item.grantfulltext | none | - |
item.openairetype | journal article | - |
item.openairecristype | http://purl.org/coar/resource_type/c_6501 | - |
item.cerifentitytype | Publications | - |
crisitem.author.dept | Clinical Laboratory Sciences and Medical Biotechnology | - |
crisitem.author.dept | Clinical Laboratory Sciences and Medical Biotechnology | - |
crisitem.author.dept | Pathology | - |
crisitem.author.dept | Medical Device and Imaging | - |
crisitem.author.dept | Clinical Laboratory Sciences and Medical Biotechnology | - |
crisitem.author.orcid | 0000-0002-8800-8474 | - |
crisitem.author.orcid | 0000-0003-4535-9036 | - |
crisitem.author.orcid | 0000-0003-0104-741X | - |
crisitem.author.parentorg | College of Medicine | - |
crisitem.author.parentorg | College of Medicine | - |
crisitem.author.parentorg | College of Medicine | - |
crisitem.author.parentorg | College of Medicine | - |
crisitem.author.parentorg | College of Medicine | - |
顯示於: | 醫學檢驗暨生物技術學系 |
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